Cu2+-RGDFRGDS: exploring the mechanism and&amp;nbsp;high efficacy of the nanoparticle in antithrombotic therapy

Wu, Jianhui; Wang, Yuji; Wang, Yaonan; Zhao, Ming; Zhang, Xiaoyi; Gui, Lin; Zhao, Shunying; Zhu, Haimei; Zhao, Jinghua; Peng, Shiqi

doi:10.2147/ijn.s76691

Cited by 7 publications

(3 citation statements)

References 38 publications

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“…The mixture was stirred at room temperature for 24 hours in acetate buffer (pH 4.7). [34][35][36][37][38] After the reaction, the pH of the solution was adjusted to a value of 9.0 by NaOH and the product was collected, centrifuged (125 g, 15 minutes), and washed with DI water three times. Eventually, GPF was obtained and freeze dried.…”

Section: Introductionmentioning

confidence: 99%

Doxorubicin and anti-VEGF siRNA co-delivery via nano-graphene oxide for enhanced cancer therapy in vitro and in vivo

Sun¹,

Wang²,

Cui³

et al. 2018

IJN

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BackgroundGraphene oxide (GO) has attracted intensive interest in biological and medical fields in recent years due to its unique physical, chemical, and biological properties. In our previous work, we proved that GO could deliver small interfering RNA (siRNA) into cells and downregulate the expression of the desired gene.MethodsThis study investigated the potential of a modified GO nanocarrier for co-delivery of siRNA and doxorubicin (DOX) for enhanced cancer therapy. Fourier transform infrared spectroscopy, laser particle size analyzer, UV-visible spectroscopy, gel electrophoresis retardation, and in vitro release assay were studied.ResultsThe results of real-time polymerase chain reaction revealed that the expression of vascular endothelial growth factor (VEGF) mRNA was decreased 46.84%±3.72% (mean ± SD). Enzyme-linked immunosorbent assay indicated that the expression of VEGF protein was down-regulated to 52.86%±1.10% (mean ± SD) in vitro. In vivo tumor growth assay GO-poly-l-lysine hydrobromide/folic acid (GPF)/DOX/siRNA exhibited gene silencing and tumor inhibition (66.95%±2.35%, mean ± SD) compared with naked siRNA (1.62%±1.47%, mean ± SD) and DOX (33.63%±5.85%, mean ± SD). GPF/DOX/siRNA exhibited no testable cytotoxicity.ConclusionThe results indicated that co-delivery of siRNA and DOX by GPF could be a promising application in tumor clinical therapy.

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Section: Introductionmentioning

confidence: 99%

Doxorubicin and anti-VEGF siRNA co-delivery via nano-graphene oxide for enhanced cancer therapy in vitro and in vivo

Sun¹,

Wang²,

Cui³

et al. 2018

IJN

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“…Since the particles of 100 nm in diameter have minimal probability of being entrapped by macrophages in blood circulation, 37 the AFM images of small molecules in rat plasma were recorded in particular to simulate the feature of nanoparticles in blood circulation. 34 – 36 The AFM images and the diameters of RGDF-Dex nanoparticles (close to 100 nm) shown in Figure 3 suggest that it can be safely delivered in blood circulation.…”

Section: Discussionmentioning

confidence: 94%

RGD(F/S/V)-Dex: towards the development of novel, effective, and safe glucocorticoids

Jiang

Zhao

Wang

et al. 2016

DDDT

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Dexamethasone (Dex) is an effective glucocorticoid in treating inflammation and preventing rejection reaction. However, the side effects limit its clinical application. To improve its druggable profile, the conjugates of RGD-peptide-modified Dex were presented and their enhanced anti-inflammation activity, minimized osteoporotic action, and nanoscaled assembly were explored. (RGD stands for Arg-Gly-Asp. Standard single letter biochemical abbreviations for amino acids have been used throughout this paper.) In respect of the rejection reaction, the survival time of the implanted myocardium of the mice treated with 1.43 µmol/kg/d of the conjugates for 15 consecutive days was significantly longer than that of the mice treated with 2.5 µmol/kg/d of Dex, and the conjugates, but not Dex, exhibited no toxic action. At a single dose of 14.3 µmol/kg (100 times minimal effective dose, 0.143 µmol/kg), the conjugates induced no liver, kidney, or systemic toxicity. At the dose of 1.43 µmol/kg, the conjugates, but not Dex, prolonged the bleeding time of the mice, and inhibited the thrombosis of the rats. In water and rat plasma, the conjugates formed nanoparticles of 14–250 and 101–166 nm in diameter, respectively. Since the nanoparticles of ~100 nm in size cannot be entrapped by macrophages in the circulation, RGDF-Dex would particularly be worthy of development, since its nanoparticle diameter is 101 nm.

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“…The self-assembly of small molecule has been well documented 29,37. Here the self-assembly of BCESA in ultrapure water (1 nM) was explored with its FT-MS spectrum.…”

Section: Resultsmentioning

confidence: 99%

<p>BCESA: a nano-scaled intercalator capable of targeting tumor tissue and releasing anti-tumoral β-carboline-3-carboxylic acid</p>

Cui

Zhang

et al. 2019

IJN

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Background: In the discovery of DNA intercalators, β-carbolines compose one member of the most interesting alkaloid family and are of clinical importance. In the efforts, N-(3-benzyloxycarbonyl-β-carboline-1-yl)ethyl-Ser-Ala-OBzl (BCESA) was designed as a nano-scaled DNA intercalator without Dox-like toxicity. Methods: Based on the structural analysis and CDOCKER energy comparison, BCESA was rationally designed as such a nano-scaled intercalator. The anti-tumor activity, the toxicity and the tumor targeting action of BCESA were evaluated on mouse models. Results: The in vitro proliferation of cancer cells, but not non-cancer cells, was effectively inhibited by BCESA. On S180 mouse model BCESA dose-dependently slowed the tumor growth, and 0.01 μmol/kg/day was found as a minimal effective dose. Both BCESA and its moiety were found in the tumor tissue, but not in the organs and the blood, of S180 mice. Conclusion: BCESA should be a nano-scaled intercalator capable of targeting tumor tissue to release anti-tumoral β-carboline-3-carboxylic acid and its 1-methyl derivative, while Ser-Ala-OBzl is a simple and desirable carrier.

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Cu2+-RGDFRGDS: exploring the mechanism and high efficacy of the nanoparticle in antithrombotic therapy

Cited by 7 publications

References 38 publications

Doxorubicin and anti-VEGF siRNA co-delivery via nano-graphene oxide for enhanced cancer therapy in vitro and in vivo

Doxorubicin and anti-VEGF siRNA co-delivery via nano-graphene oxide for enhanced cancer therapy in vitro and in vivo

RGD(F/S/V)-Dex: towards the development of novel, effective, and safe glucocorticoids

<p>BCESA: a nano-scaled intercalator capable of targeting tumor tissue and releasing anti-tumoral β-carboline-3-carboxylic acid</p>

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Cu2+-RGDFRGDS: exploring the mechanism and&nbsp;high efficacy of the nanoparticle in antithrombotic therapy

Cited by 7 publications

References 38 publications

Doxorubicin and anti-VEGF siRNA co-delivery via nano-graphene oxide for enhanced cancer therapy in vitro and in vivo

Doxorubicin and anti-VEGF siRNA co-delivery via nano-graphene oxide for enhanced cancer therapy in vitro and in vivo

RGD(F/S/V)-Dex: towards the development of novel, effective, and safe glucocorticoids

<p>BCESA: a nano-scaled intercalator capable of targeting tumor tissue and releasing anti-tumoral &beta;-carboline-3-carboxylic acid</p>

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Cu2+-RGDFRGDS: exploring the mechanism and high efficacy of the nanoparticle in antithrombotic therapy

<p>BCESA: a nano-scaled intercalator capable of targeting tumor tissue and releasing anti-tumoral β-carboline-3-carboxylic acid</p>